Discipline of Chemistry, Indian Institute of Technology Indore , Simrol, Indore, 452020 Madhya Pradesh, India.
J Org Chem. 2016 May 20;81(10):4378-85. doi: 10.1021/acs.joc.6b00472. Epub 2016 May 6.
An interesting domino reaction of 5-membered cyclic sulfamidate imines with a variety of Morita-Baylis-Hillman acetates of nitroolefins/nitrodienes in the presence of DABCO as an organic base at 55 °C is reported for the first time. This new synthetic strategy provides a series of pharmacologically interesting 4,6-diarylpicolinates in high to excellent yields and allows several compatible functionalities on aryl rings. Moreover, the biologically interesting imidazo[1,2-a]pyridine (alpidem derivative) has been prepared in high chemical yield through a unique procedure.
首次报道了在 DABCO 作为有机碱的存在下，5-员环状磺酰胺亚胺与各种 Morita-Baylis-Hillman 硝基亚油酸酯/硝二烯的有趣的级联反应，反应温度为 55°C。这种新的合成策略提供了一系列具有药理学意义的 4,6-二芳基吡啶酸盐，产率高至优异，并允许芳环上具有多种兼容的官能团。此外，通过独特的方法制备了具有生物意义的咪唑并[1,2-a]吡啶（阿普唑仑衍生物），产率高。
